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雌激素通过G蛋白偶联机制调节印度红蝎毒液诱导的体外心房心动过缓。

Estrogen modulates in vitro atrial bradycardia induced by Indian red scorpion venom via G-protein coupled mechanisms.

作者信息

Alex Anitha B, Kanoo Sadhana, Deshpande Shripad B

机构信息

Department of Physiology, Institute of Medical Sciences, Banaras Hindu University, Varanasi-221 005, India.

出版信息

Eur J Pharmacol. 2006 Sep 28;546(1-3):102-8. doi: 10.1016/j.ejphar.2006.06.056. Epub 2006 Jun 30.

Abstract

Role of estrogen on cardiac dysrhythmia produced by Indian red scorpion (Mesobuthus tamulus) venom was examined using rat right atrial preparations in vitro. In females, the M. tamulus venom produced an increase, a decrease and an increase in rate at 0.03, 0.3 and 3 microg/ml of venom, respectively, producing N-shaped response curve, whereas no such response pattern was observed in males. Force of contraction in females was increased at all the concentrations of the venom, while in males the increase was seen only at 3 microg/ml. Castration of male rats did not alter the venom response to female type, while 'estrogenisation of castrated male rats' (pseudofemales) produced a response similar to females. Tamoxifen reversed the venom-induced responses both in females and pseudofemales. Further in females, the venom action at 0.3 microg/ml was blocked by atropine. Response at this concentration was also blocked by pertussis toxin and methylene blue. Results suggest that the cholinergic component of venom response is modulated by estrogen receptors via G(i)-protein-guanylyl cyclase mechanism.

摘要

利用大鼠离体右心房标本,研究了雌激素对印度红蝎(Mesobuthus tamulus)毒液所致心律失常的作用。在雌性大鼠中,印度红蝎毒液在毒液浓度为0.03、0.3和3微克/毫升时分别使心率增加、降低和再次增加,呈现N形反应曲线,而在雄性大鼠中未观察到这种反应模式。在所有毒液浓度下,雌性大鼠的收缩力均增加,而雄性大鼠仅在毒液浓度为3微克/毫升时收缩力增加。切除雄性大鼠睾丸并未改变其对毒液的反应类型,而对去势雄性大鼠(假雌性)进行“雌激素化”则产生了与雌性大鼠相似的反应。他莫昔芬可逆转雌性大鼠和假雌性大鼠中由毒液诱导的反应。此外,在雌性大鼠中,0.3微克/毫升毒液的作用可被阿托品阻断。该浓度下的反应也可被百日咳毒素和亚甲蓝阻断。结果表明,毒液反应的胆碱能成分通过雌激素受体经由G(i)蛋白-鸟苷酸环化酶机制进行调节。

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